Some new 2,3,6-trisubstituted quinazolinones as potent anti-inflammatory, analgesic and COX-II inhibitors

Various 2-(substitutedphenylmethyleneimino)aminoacetylmethylene-3-(2'-substitutedindol-3'-yl)-halosubstituted-4(3H)quinazolinones (5a-5i) and 2-(substituted phenylaminomethyleneacetyl-4'-oxo-1'-thiazolidinyl-3-(2"-substitutedindol-3"-yl) 4(3H)-quinazolinones (6a-6i) hav...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2003-11, Vol.11 (23), p.5293-5299
Main Authors: KUMAR, Ashok, SHARMA, Shalabh, ARCHANA, BAJAJ, Kiran, SHARMA, Shipra, PANWAR, Hemant, SINGH, Tripti, SRIVASTAVA, V. K
Format: Article
Language:English
Subjects:
Analgesics
Anti-Inflammatory Agents, Non-Steroidal - chemistry
Anti-Inflammatory Agents, Non-Steroidal - pharmacology
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Cyclooxygenase 2
Cyclooxygenase 2 Inhibitors
Cyclooxygenase Inhibitors - chemistry
Cyclooxygenase Inhibitors - pharmacology
Isoenzymes - drug effects
Magnetic Resonance Spectroscopy
Medical sciences
Neuropharmacology
Pharmacology. Drug treatments
Prostaglandin-Endoperoxide Synthases - drug effects
Quinazolines - chemistry
Quinazolines - pharmacology
Spectrophotometry, Infrared
Spectrum Analysis
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Summary:Various 2-(substitutedphenylmethyleneimino)aminoacetylmethylene-3-(2'-substitutedindol-3'-yl)-halosubstituted-4(3H)quinazolinones (5a-5i) and 2-(substituted phenylaminomethyleneacetyl-4'-oxo-1'-thiazolidinyl-3-(2"-substitutedindol-3"-yl) 4(3H)-quinazolinones (6a-6i) have been synthesized in the present studies. The structure of these compounds have been elucidated by elemental (C, H, N) and spectral (IR, 1H NMR and mass) analysis. Furthermore, above said compounds were evaluated for their anti-inflammatory, analgesic, ulcerogenic activities and acute toxicity study. Compound 6d was found to be most potent. Compound exihibiting less ulcerogenic liability and ALD(50) >2000mg/kg po.
ISSN:0968-0896
1464-3391
DOI:10.1016/s0968-0896(03)00501-7